BRD9 degrader CFT8634
Term · Oncology and biomedicine · MLC-T-ONC-012107
An orally bioavailable heterobifunctional protein degrader of bromodomain-containing protein 9 (BRD9; sarcoma antigen NY-SAR-29; rhabdomyosarcoma antigen MU-RMS-40.8), with potential antineoplastic activity. CFT8634 is comprised of an E3 ligase-binding moiety and a BRD9-binding moiety. Upon oral administration, BRD9 degrader CFT8634 targets and binds to BRD9 with its BRD9-binding moiety. Upon BRD9 binding, the E3 ligase-binding moiety binds to cereblon (CRBN), a component of the CRL4-CRBN E3 ubiquitin ligase complex, which directs proteins for destruction, resulting in the proteasome-mediated degradation of BRD9. This leads to an inhibition of the growth of tumor cells that rely on BRD9 for survival. BRD9, a component of one form of the Brg/Brahma-Associated Factor (BAF) complex, is needed for the survival of certain cancer cells due to mutations.
| Identifier | MLC-T-ONC-012107 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | BRD9-targeting protein degrader CFT8634; BiDAC degrader CFT8634; BRD9 protein degrader CFT8634; bifunctional degradation activating compound CFT8634 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-012107",
"term": "BRD9 degrader CFT8634",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable heterobifunctional protein degrader of bromodomain-containing protein 9 (BRD9; sarcoma antigen NY-SAR-29; rhabdomyosarcoma antigen MU-RMS-40.8), with potential antineoplastic activity. CFT8634 is comprised of an E3 ligase-binding moiety and a BRD9-binding moiety. Upon oral administration, BRD9 degrader CFT8634 targets and binds to BRD9 with its BRD9-binding moiety. Upon BRD9 binding, the E3 ligase-binding moiety binds to cereblon (CRBN), a component of the CRL4-CRBN E3 ubiquitin ligase complex, which directs proteins for destruction, resulting in the proteasome-mediated degradation of BRD9. This leads to an inhibition of the growth of tumor cells that rely on BRD9 for survival. BRD9, a component of one form of the Brg/Brahma-Associated Factor (BAF) complex, is needed for the survival of certain cancer cells due to mutations.",
"synonyms": [
"BRD9-targeting protein degrader CFT8634",
"BiDAC degrader CFT8634",
"BRD9 protein degrader CFT8634",
"bifunctional degradation activating compound CFT8634"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/brd9-degrader-cft8634/"
}
Record 3,819 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.